Abstract:

The present invention is generally directed to the treatment of fine
wrinkles, hyperpigmentation, roughness of facial skin, improvement of
photoaging, repair of sun damaged skin, and related disorders. In a
formulation aspect, the present invention provides a formulation for the
adjunct treatment of skin disorders, where the formulation includes
tretinoin and azelaic acid. In a method aspect, the present invention
provides a method for treating skin disorders. The skin disorders include
fine wrinkles, freckles, solar lentigo, skin photodamage, aging process
as reflected by changes in a patient's skin, Acne Vulgaris and Melasma or
Post-inflammatory hyperpigmentation. The method includes the application
of a formulation to a portion of the patient's skin, where the portion
exhibits a skin disorder, and wherein the formulation includes tretinoin
and azelaic acid.

Claims:

1. A formulation for the adjunct treatment of skin disorders, wherein the
formulation comprises tretinoin and azelaic acid.

2. The formulation according to claim 1, wherein the concentration of
tretinoin in the formulation is at least 0.01%.

3. The formulation according to claim 2, wherein the concentration of
azelaic acid in the formulation is at least 7.5%.

4. The formulation according to claim 3, wherein the concentration of
tretinoin in the formulation is at least 0.02% and the concentration of
azelaic acid in the formulation is at least 10.0%.

5. The formulation according to claim 4, wherein the concentration of
tretinoin in the formulation does not exceed 10%.

6. The formulation according to claim 5, wherein the concentration of
azelaic acid in the formulation does not exceed 30%.

7. The formulation according to claim 6, wherein the formulation is a
solution, gel, cream, emollient, foam, ointment, lotion, shampoo or
spray.

8. The formulation according to claim 7, wherein the formulation is a
fragrance free, alcohol free, water-based gel.

9. The formulation according to claim 8, wherein the formulation further
comprises fluocinolone acetonide.

10. A method for treating skin disorders, wherein the skin disorders
include fine wrinkles, freckles, solar lentigo, skin photodamage, aging
process as reflected by changes in a patient's skin, Acne Vulgaris and
Melasma or Post-inflammatory hyperpigmentation, and wherein the method
comprises the application of a formulation to a portion of the patient's
skin, and wherein the portion exhibits a skin disorder, and wherein the
formulation comprises tretinoin and azelaic acid.

Description:

[0001]This application claims the benefit of U.S. provisional patent
application No. 61/214,640, filed Apr. 27, 2009, the entire contents of
which are incorporated herein by reference.

[0003]RENOVA® (tretinoin cream) 0.05% is an adjunctive agent for use in
the mitigation (palliation) of fine wrinkles, mottled hyperpigmentation
and tactile roughness of facial skin in patients who use comprehensive
skin care and sunlight avoidance programs. RENOVA® does not eliminate
wrinkles, repair sun damaged skin, reverse photoaging, or restore more
youthful or younger skin. In double-blinded, vehicle-controlled clinical
studies, many patients in the vehicle group achieved palliative effects
on fine wrinkling, mottled hyperpigmentation, and tactile roughness of
facial skin with the use of comprehensive skin care and sunlight
avoidance programs including sunscreens, protective clothing, and
non-prescription emollient creams.

[0004]RENOVA 0.05% has not demonstrated a mitigating effect on deep
wrinkling, skin yellowing, lentigines, telangiectasia, skin laxity,
keratinocyte atypia, melanocytic atypia or dermal elastosis, which are
oftentimes the result of chronic sun exposure. The effectiveness of
RENOVA 0.05% for mitigating fine wrinkles, mottled hyperpigmentation and
tactile roughness of facial skin has not been established in people
greater than 50 years of age.

[0005]There is a need for improved compounds, formulations and methods
that can address the same indications as RENOVA.

[0007]In a formulation aspect, the present invention provides a
formulation for the adjunct treatment of skin disorders, where the
formulation includes tretinoin and azelaic acid.

[0008]In a method aspect, the present invention provides a method for
treating skin disorders. The skin disorders include fine wrinkles,
freckles, solar lentigo, skin photodamage, aging process as reflected by
changes in a patient's skin, Acne Vulgaris and Melasma or
Post-inflammatory hyperpigmentation. The method includes the application
of a formulation to a portion of the patient's skin, where the portion
exhibits a skin disorder, and wherein the formulation includes tretinoin
and azelaic acid.

DETAILED DESCRIPTION OF THE INVENTION

[0009]The present invention is generally directed to the treatment of fine
wrinkles, hyperpigmentation, roughness of facial skin, improvement of
photoaging, repair of sun damaged skin, and related disorders. It is more
specifically directed to formulations that include both tretinoin and
azelaic acid, which are used to treat a patient's skin.

[0010]Formulations according to the present invention are typically in one
of the following forms: solution, gel (e.g., water-based), cream,
emollient, foam, ointment, lotion, shampoo, or spray. In one embodiment
the formulation is a fragrance free, alcohol free, water-based gel.

[0011]Tretinoin is included in the formulations at a concentration of at
least 0.005%. Oftentimes it is included in the formulations at a
concentration of at least 0.01%, 0.015%, 0.02%, 0.025%, 0.03%, 0.035%,
0.040%, 0.045%, 0.050%, 0.055%, 0.060%, 0.065%, 0.070%, 0.075%, 0.080%,
0.085%, 0.090%, 0.095%, or 0.10%. Tretinoin concentration in the
formulations typically does not exceed 0.5%, and it usually does not
exceed 0.45%, 0.40%, 0.35%, 0.30%, 0.25%, 0.20%, 0.15%, 0.10%, or 0.05%.

[0012]Azelaic acid is included in the formulations at a concentration of
at least 5%. It is oftentimes included in the formulations at a
concentration of at least 7.5%, 10.0%, 12.5%, 15.0%, 17.5%, 20.0%, 22.5%,
25.0%, 27.5%, or 30.0%. Azelaic acid concentration in the formulations
typically does not exceed 50.0%, and it usually does not exceed 47.5%,
45.0%, 42.5%, 40.0%, 37.5%, 35.0%, 32.50%, 30.0%, 27.50%, 25.0%, 22.5%,
or 20%.

[0013]Preferred formulations according to the present invention include
about 0.02% tretinoin and about 15% azelaic acid or about 0.05% tretinoin
and 15% azelaic acid.

[0015]Formulations of the present invention may be used to treat at least
the following conditions: fine wrinkles, freckles, solar lentigo, skin
photodamage, aging process as reflected by changes in a patient's skin,
Acne Vulgaris and Melasma and Post-inflammatory hyperpigmentation.

[0016]The formulation is typically applied once daily, although
application of the formulation more than once daily may be advisable for
certain indications.

[0017]From the foregoing it will be appreciated that, although specific
embodiments of the invention have been described herein for purposes of
illustration, various modifications may be made without deviating from
the spirit and scope of the invention. Accordingly, the invention is not
limited except as by the appended claims.